HIF-1/2α-IN-1
HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .
For research use only. We do not sell to patients.
- CAS No.: 2827693-99-0
- Formula: C17H16N6O4
- Molecular Weight:368.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HIF-2α 0.92 μM (IC50) |
HIF-1/2α-IN-1 (compound #25) (0.01-100 μM) inhibits HIF-2α activity with an IC50 value of 0.92 μM[1].
HIF-1/2α-IN-1 (0-10 μM, 24 h) decrease HIF-2α by inhibiting IRE-dependent translation and also inhibit HIF-1α at higher concentrations，which effects mediates by inhibiting the function of iron sulfur cluster assembly 2 (ISCA2) [1].
HIF-1/2α-IN-1 (1 μM, 24 h) targets ISCA2 and trigger the iron starvation response[1].
HIF-1/2α-IN-1 (0-100 μM, 24 h) decreased cell viability in 786-0 cells (IC50=1.7 μM (786-0), 10.6 μM (786-0 VHL)) and RCC4 cells (IC50=4.8 μM (RCC4), 71.0 μM (RCC4 VHL)) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:786-0 cells and RCC4 cells
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Concentration:0.01-100 μM
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Incubation Time:24 h
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Result:Decreased cell viability in 786-0 cells and RCC4 cells.
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Cell Line:786-0 cells and RCC10 cells
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Concentration:0, 0.5, 1, 2.5, 10 μM
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Incubation Time:24 h
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Result:Decreased HIF-2α activity and protein levels.
Decreased HIF-1α levels at higher concentrations or treatment durations, but do not promote proteasomal degradation of HIF-1/2α.
Inhibited the production of luciferase driven by the HIF-2α IRE (IRE-Luc).
Increasesed IRP2, TFRC in dose-dependent and decreased FTH.
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Cell Line:786-0 cells
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Concentration:0, 0.5, 1, 5 μM
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Incubation Time:24 h
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Result:Resulted in a dose-dependent decrease in the transcription of HIF-2α target genes VEGFA and POU5F1, but not inhibited HIF-2α transcription.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NRG or Balb/c mice[1]
(6-8 week old, male, 10 per group) -
Dosage:30, 60 mg/kg
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Administration:p.o., daily
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Result:Significantly inhibited tumor growth.
Had well tolerated with no significant weight loss.
Chemical Information
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CAS No. 2827693-99-0
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Molecular Weight 368.35
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Formula C17H16N6O4
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SMILES
COC1=CC=C(C=C1OC)C2=NN=C(O2)NC3=NC4=C(N3)C=CN=C4OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HIF-1/2α-IN-1 Related Classifications
HY-151341 Related Classifications
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